Identification
- Brand Names
- Renese-R
- Generic Name
- Reserpine
- DrugBank Accession Number
- DB00206
- Background
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
The FDA withdrew its approval for the use of all oral dosage form drug products containing more than 1 mg of reserpine.6
- Type
- Small Molecule
- Groups
- Approved, Investigational, Withdrawn
- Structure
Structure for Reserpine (DB00206)
- Weight
- Average: 608.6787
Monoisotopic: 608.273380888 - Chemical Formula
- C33H40N2O9
- Synonyms
- (−)-reserpine
- (3beta,16beta,17alpha,18beta,20alpha)-11,17-Dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylic acid methyl ester
- 3,4,5-trimethoxybenzoyl methyl reserpate
- Reserpin
- Reserpine
- External IDs
- ENT-50146
- NSC-237659
- NSC-59272
Pharmacology
- Indication
For the treatment of hypertension
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to manage Hypertension Combination Product in combination with: Polythiazide (DB01324) •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Reserpine is an adrenergic blocking agent used to treat mild to moderate hypertension via the disruption of norepinephrine vesicular storage. The antihypertensive actions of Reserpine are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral resistance.
- Mechanism of action
Reserpine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.
Target Actions Organism ASynaptic vesicular amine transporter inhibitorHumans UChromaffin granule amine transporter inhibitorHumans UBaculoviral IAP repeat-containing protein 5 Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
62%
- Metabolism
- Not Available
- Route of elimination
Reserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Possible human carcinogen. May cause reproductive harm. ORL-RAT LD50 420 mg/kg; IPR-RAT LD50 44 mg/kg; IVN-RAT LD50 15 mg/kg; ORL-MUS LD50 200 mg/kg; SCU-MUS LD50 52 mg/kg; IPR-RBT LD50 7 mg/kg
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Reserpine is combined with 1,2-Benzodiazepine. Abacavir Reserpine may decrease the excretion rate of Abacavir which could result in a higher serum level. Abaloparatide The risk or severity of adverse effects can be increased when Reserpine is combined with Abaloparatide. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Reserpine. Acebutolol Reserpine may increase the hypotensive activities of Acebutolol. - Food Interactions
- Avoid alcohol.
- Take with food. Food reduces irritation.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Apoplon / Hiserpia / Novoreserpine / Reserfia / Serpalan / Serpanray / Serpasil
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Reserpine Tablet 0.1 mg/1 Oral Eon Labs, Inc. 1988-03-11 2013-07-31 US 
Reserpine Tablet 0.25 mg/1 Oral Physicians Total Care, Inc. 1988-03-11 2002-06-30 US Reserpine Tablet 0.25 mg/1 Oral Eon Labs, Inc. 1988-03-11 2013-07-31 US Reserpine Tablet 0.1 mg/1 Oral Physicians Total Care, Inc. 1988-03-11 2002-06-30 US Serpasil 0.25mg Tablet 0.25 mg / tab Oral Novartis 1954-12-31 1999-08-04 Canada 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Novo-reserpine Tab 0.25mg Tablet .25 mg Oral Novopharm Limited 1967-12-31 2005-08-10 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Diupres Reserpine (0.125 mg/1) + Chlorothiazide (500 mg/1) Tablet Oral Merck & Co., Inc. 2006-03-02 2006-07-13 US Diupres Reserpine (0.125 mg/1) + Chlorothiazide (250 mg/1) Tablet Oral Merck & Co., Inc. 2006-03-02 2006-07-13 US Hydropres 25 Tab Reserpine (.125 mg) + Hydrochlorothiazide (25 mg) Tablet Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1959-12-31 2000-06-14 Canada Hydropres 50 Tab Reserpine (.125 mg) + Hydrochlorothiazide (50 mg) Tablet Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1959-12-31 1998-08-14 Canada REGROTON TABLET, 20 ADET Reserpine (0.25 mg) + Chlorthalidone (50 mg) Tablet Oral ASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş. 2011-06-24 Not applicable Turkey 
Categories
- ATC Codes
- C02LA51 — Reserpine and diuretics, combinations with other drugs
- C02LA — Rauwolfia alkaloids and diuretics in combination
- C02L — ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
- C02 — ANTIHYPERTENSIVES
- C — CARDIOVASCULAR SYSTEM
- C02AA — Rauwolfia alkaloids
- C02A — ANTIADRENERGIC AGENTS, CENTRALLY ACTING
- C02 — ANTIHYPERTENSIVES
- C — CARDIOVASCULAR SYSTEM
- C02LA — Rauwolfia alkaloids and diuretics in combination
- C02L — ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
- C02 — ANTIHYPERTENSIVES
- C — CARDIOVASCULAR SYSTEM
- C02LA — Rauwolfia alkaloids and diuretics in combination
- C02L — ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
- C02 — ANTIHYPERTENSIVES
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Adrenergic Agents
- Adrenergic Uptake Inhibitors
- Alkaloids
- Antiadrenergic Agents, Centrally Acting
- Antidepressive Agents
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Antipsychotic Agents
- BSEP/ABCB11 Inhibitors
- Cardiovascular Agents
- Catecholamine-depleting Sympatholytic
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Decreased Sympathetic Activity
- Drugs that are Mainly Renally Excreted
- Gastrointestinal Acidifying Agents
- Heterocyclic Compounds, Fused-Ring
- Hypotensive Agents
- Indole Alkaloids
- Indoles
- Indolizidines
- Indolizines
- Membrane Transport Modulators
- Neurotoxic agents
- Neurotransmitter Agents
- Neurotransmitter Uptake Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OCT1 inhibitors
- OCT2 Substrates
- Organic Anion Transporting Polypeptide 2B1 Inhibitors
- P-glycoprotein inducers
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Psychotropic Drugs
- Secologanin Tryptamine Alkaloids
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as yohimbine alkaloids. These are alkaloids containing the pentacyclic yohimban skeleton. The Yohimbinoid alkaloids contain a carbocyclic ring E arising through C-17 to C-18 bond formation in a corynantheine precursor.
- Kingdom
- Organic compounds
- Super Class
- Alkaloids and derivatives
- Class
- Yohimbine alkaloids
- Sub Class
- Not Available
- Direct Parent
- Yohimbine alkaloids
- Alternative Parents
- Corynanthean-type alkaloids / Beta carbolines / Gallic acid and derivatives / M-methoxybenzoic acids and derivatives / P-methoxybenzoic acids and derivatives / 3-alkylindoles / Benzoic acid esters / Anisoles / Methoxybenzenes / Phenoxy compounds show 16 more
- Substituents
- 3-alkylindole / Alkyl aryl ether / Amine / Amino acid or derivatives / Anisole / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Benzoate ester show 36 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- alkaloid ester, yohimban alkaloid (CHEBI:28487) / Indole alkaloids, Alkaloids (C06539)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 8B1QWR724A
- CAS number
- 50-55-5
- InChI Key
- QEVHRUUCFGRFIF-MDEJGZGSSA-N
- InChI
- InChI=1S/C33H40N2O9/c1-38-19-7-8-20-21-9-10-35-16-18-13-27(44-32(36)17-11-25(39-2)30(41-4)26(12-17)40-3)31(42-5)28(33(37)43-6)22(18)15-24(35)29(21)34-23(20)14-19/h7-8,11-12,14,18,22,24,27-28,31,34H,9-10,13,15-16H2,1-6H3/t18-,22+,24-,27-,28+,31+/m1/s1
- IUPAC Name
- methyl (1R,15S,17R,18R,19S,20S)-6,18-dimethoxy-17-(3,4,5-trimethoxybenzoyloxy)-3,13-diazapentacyclo[11.8.0.0^{2,10}.0^{4,9}.0^{15,20}]henicosa-2(10),4(9),5,7-tetraene-19-carboxylate
- SMILES
- [H][C@]12C[C@@H](OC(=O)C3=CC(OC)=C(OC)C(OC)=C3)[C@H](OC)[C@@H](C(=O)OC)[C@@]1([H])C[C@@]1([H])N(CCC3=C1NC1=C3C=CC(OC)=C1)C2
References
- General References
- Authors unspecified: Five-year findings of the hypertension detection and follow-up program. I. Reduction in mortality of persons with high blood pressure, including mild hypertension. Hypertension Detection and Follow-up Program Cooperative Group. JAMA. 1979 Dec 7;242(23):2562-71. [Article]
- Authors unspecified: Effects of treatment on morbidity in hypertension. Results in patients with diastolic blood pressures averaging 115 through 129 mm Hg. JAMA. 1967 Dec 11;202(11):1028-34. [Article]
- Authors unspecified: Prevention of stroke by antihypertensive drug treatment in older persons with isolated systolic hypertension. Final results of the Systolic Hypertension in the Elderly Program (SHEP). SHEP Cooperative Research Group. JAMA. 1991 Jun 26;265(24):3255-64. [Article]
- Chobanian AV, Bakris GL, Black HR, Cushman WC, Green LA, Izzo JL Jr, Jones DW, Materson BJ, Oparil S, Wright JT Jr, Roccella EJ: The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: the JNC 7 report. JAMA. 2003 May 21;289(19):2560-72. Epub 2003 May 14. [Article]
- Moser M: "Cost containment" in the management of hypertension. Ann Intern Med. 1987 Jul;107(1):107-9. [Article]
- Code of Federal Regulations 216.24: Drug products withdrawn or removed from the market for reasons of safety or effectiveness. [Link]
- External Links
- Human Metabolome Database
- HMDB0014351
- KEGG Drug
- D00197
- KEGG Compound
- C06539
- PubChem Compound
- 5770
- PubChem Substance
- 46505863
- ChemSpider
- 5566
- BindingDB
- 50017712
- 9260
- ChEBI
- 28487
- ChEMBL
- CHEMBL772
- ZINC
- ZINC000003938746
- Therapeutic Targets Database
- DAP000755
- PharmGKB
- PA451236
- PDBe Ligand
- YHR
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Reserpine
- PDB Entries
- 8jtc / 8t6a
- MSDS
- Download (73.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Completed Prevention Atherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus / High Cholesterol / Hypertension / Type 2 Diabetes Mellitus 1 3 Completed Prevention Cardiovascular Disease (CVD) / Cerebrovascular Diseases / Hypertension 1 2 Completed Treatment Cardiovascular Disease (CVD) / Hypertension / Vascular Diseases 1 2 Completed Treatment Cocaine Related Disorders / Substance Related Disorders 1 2 Completed Treatment Refractory Hypertension 1
Pharmacoeconomics
- Manufacturers
- Novartis pharmaceuticals corp
- Eli lilly and co
- Bowman pharmaceuticals inc
- Bristol myers squibb co
- Barr laboratories inc
- Bell pharmacal corp
- Cm bundy co
- Elkins sinn div ah robins co inc
- Everylife
- Halsey drug co inc
- Impax laboratories inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Marshall pharmacal corp
- Mk laboratories inc
- Mylan pharmaceuticals inc
- Pharmavite pharmaceuticals
- Purepac pharmaceutical co
- Private formulations inc
- Rexall drug co
- Roxane laboratories inc
- Sandoz inc
- Solvay pharmaceuticals
- Tablicaps inc
- Teva pharmaceuticals usa inc
- Valeant pharmaceuticals international
- Watson laboratories inc
- West ward pharmaceutical corp
- Whiteworth towne paulsen inc
- Lannett co inc
- Panray corp sub ormont drug and chemical co inc
- Vale chemical co inc
- Vitarine pharmaceuticals inc
- Packagers
- Apotheca Inc.
- C.O. Truxton Inc.
- Carlisle Laboratories Inc.
- Dispensing Solutions
- Eon Labs
- H and H Laboratories
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Physicians Total Care Inc.
- Quality Research Pharmaceutical Inc.
- United Research Laboratories Inc.
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral .25 mg Tablet Oral Tablet Oral 0.1 mg/1 Tablet Oral 0.25 mg/1 Tablet, coated Oral Tablet Oral 0.25 mg / tab Tablet, sugar coated Oral - Prices
Unit description Cost Unit Reserpine 0.25 mg tablet 1.52USD tablet Reserpine 0.1 mg tablet 0.83USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 264.5 °C PhysProp water solubility 73 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 3.2 Not Available pKa 6.6 MERCK INDEX (1996) - Predicted Properties
Property Value Source Water Solubility 0.0113 mg/mL ALOGPS logP 4.05 ALOGPS logP 3.53 Chemaxon logS -4.7 ALOGPS pKa (Strongest Acidic) 16.29 Chemaxon pKa (Strongest Basic) 7.39 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 117.78 Å2 Chemaxon Rotatable Bond Count 10 Chemaxon Refractivity 161.42 m3·mol-1 Chemaxon Polarizability 66.06 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9216 Blood Brain Barrier + 0.9257 Caco-2 permeable + 0.6549 P-glycoprotein substrate Substrate 0.7928 P-glycoprotein inhibitor I Inhibitor 0.8563 P-glycoprotein inhibitor II Non-inhibitor 0.75 Renal organic cation transporter Inhibitor 0.5194 CYP450 2C9 substrate Non-substrate 0.8859 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7065 CYP450 1A2 substrate Inhibitor 0.8965 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.9384 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.831 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7062 Ames test Non AMES toxic 0.9132 Carcinogenicity Non-carcinogens 0.9439 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.1297 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7505 hERG inhibition (predictor II) Non-inhibitor 0.6194
Spectra
- Mass Spec (NIST)
- Download (10.3 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 275.5426226 predictedDarkChem Lite v0.1.0 [M-H]- 278.3527226 predictedDarkChem Lite v0.1.0 [M-H]- 269.1977226 predictedDarkChem Lite v0.1.0 [M-H]- 273.6964226 predictedDarkChem Lite v0.1.0 [M-H]- 225.2428 predictedDeepCCS 1.0 (2019) [M+H]+ 275.8853226 predictedDarkChem Lite v0.1.0 [M+H]+ 278.3008226 predictedDarkChem Lite v0.1.0 [M+H]+ 270.3487226 predictedDarkChem Lite v0.1.0 [M+H]+ 272.6361226 predictedDarkChem Lite v0.1.0 [M+H]+ 227.0677 predictedDeepCCS 1.0 (2019) [M+Na]+ 275.9187226 predictedDarkChem Lite v0.1.0 [M+Na]+ 260.9394518 predictedDarkChem Lite v0.1.0 [M+Na]+ 269.1607226 predictedDarkChem Lite v0.1.0 [M+Na]+ 232.67351 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Monoamine transmembrane transporter activity
- Specific Function
- Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
- Gene Name
- SLC18A2
- Uniprot ID
- Q05940
- Uniprot Name
- Synaptic vesicular amine transporter
- Molecular Weight
- 55712.075 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Sievert MK, Hajipour AR, Ruoho AE: Specific derivatization of the vesicle monoamine transporter with novel carrier-free radioiodinated reserpine and tetrabenazine photoaffinity labels. Anal Biochem. 2007 Aug 1;367(1):68-78. Epub 2007 May 3. [Article]
- Naudon L, Leroux-Nicollet I, Raisman-Vozari R, Botton D, Costentin J: Time-course of modifications elicited by reserpine on the density and mRNA synthesis of the vesicular monoamine transporter, and on the density of the membrane dopamine uptake complex. Synapse. 1995 Sep;21(1):29-36. [Article]
- Erickson JD, Eiden LE, Hoffman BJ: Expression cloning of a reserpine-sensitive vesicular monoamine transporter. Proc Natl Acad Sci U S A. 1992 Nov 15;89(22):10993-7. [Article]
- Mandela P, Chandley M, Xu YY, Zhu MY, Ordway GA: Reserpine-induced reduction in norepinephrine transporter function requires catecholamine storage vesicles. Neurochem Int. 2010 May-Jun;56(6-7):760-7. doi: 10.1016/j.neuint.2010.02.011. Epub 2010 Feb 20. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Serotonin transmembrane transporter activity
- Specific Function
- Involved in the transport of biogenic monoamines, such as serotonin, from the cytoplasm into the secretory vesicles of neuroendocrine and endocrine cells.
- Gene Name
- SLC18A1
- Uniprot ID
- P54219
- Uniprot Name
- Chromaffin granule amine transporter
- Molecular Weight
- 56256.71 Da
References
- Ashe KM, Chiu WL, Khalifa AM, Nicolas AN, Brown BL, De Martino RR, Alexander CP, Waggener CT, Fischer-Stenger K, Stewart JK: Vesicular monoamine transporter-1 (VMAT-1) mRNA and immunoreactive proteins in mouse brain. Neuro Endocrinol Lett. 2011;32(3):253-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Multitasking protein that has dual roles in promoting cell proliferation and preventing apoptosis. Component of a chromosome passage protein complex (CPC) which is essential for chromosome alignmen...
- Gene Name
- BIRC5
- Uniprot ID
- O15392
- Uniprot Name
- Baculoviral IAP repeat-containing protein 5
- Molecular Weight
- 16388.555 Da
References
- Wang Z, Guo X, Liu Z, Cui M, Song F, Liu S: Studies on alkaloids binding to GC-rich human survivin promoter DNA using positive and negative ion electrospray ionization mass spectrometry. J Mass Spectrom. 2008 Mar;43(3):327-35. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitorInducer
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Geick A, Eichelbaum M, Burk O: Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001 May 4;276(18):14581-7. Epub 2001 Jan 31. [Article]
- Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [Article]
- Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [Article]
- Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [Article]
- Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):765-72. [Article]
- Horie K, Tang F, Borchardt RT: Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter. Pharm Res. 2003 Feb;20(2):161-8. [Article]
- Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [Article]
- Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [Article]
- Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Grundemann D, Gorboulev V, Gambaryan S, Veyhl M, Koepsell H: Drug excretion mediated by a new prototype of polyspecific transporter. Nature. 1994 Dec 8;372(6506):549-52. [Article]
- Breidert T, Spitzenberger F, Grundemann D, Schomig E: Catecholamine transport by the organic cation transporter type 1 (OCT1). Br J Pharmacol. 1998 Sep;125(1):218-24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [Article]
- Lecureur V, Sun D, Hargrove P, Schuetz EG, Kim RB, Lan LB, Schuetz JD: Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. Mol Pharmacol. 2000 Jan;57(1):24-35. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):773-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- Grundemann D, Koster S, Kiefer N, Breidert T, Engelhardt M, Spitzenberger F, Obermuller N, Schomig E: Transport of monoamine transmitters by the organic cation transporter type 2, OCT2. J Biol Chem. 1998 Nov 20;273(47):30915-20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
- Gene Name
- SLCO2B1
- Uniprot ID
- O94956
- Uniprot Name
- Solute carrier organic anion transporter family member 2B1
- Molecular Weight
- 76709.98 Da
References
- Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [Article]
Drug created at June 13, 2005 13:24 / Updated at January 02, 2024 23:43